TCRS-417 (T417) is a small-molecular inhibitor for PBX1 . TCRS-417 can directly block PBX1-binding to DNA ( IC 50 = 6.58 μM), and affects PBX1 transcription. TCRS-417 is able to hammer out the stemness traits of Carboplatin ( HY-17393 )-resistant (CR) cells to revert to a differentiated status through tacking PBX1 signaling cascade. TCRS-417 significantly suppresses self-renewal and proliferation of cancer cells expressing high levels of PBX1. TCRS-417 can decrease the mRNA levels of FOXM1 , NEK2 , and E2F2 in cancer cell lines. TCRS-417 is selectively toxic against chr1q-amp myeloma and solid tumor cells.
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